CN101618178A - Application of curcuma extract in preparation of medicament for treating Parkinson's disease - Google Patents
Application of curcuma extract in preparation of medicament for treating Parkinson's disease Download PDFInfo
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- CN101618178A CN101618178A CN200810115852A CN200810115852A CN101618178A CN 101618178 A CN101618178 A CN 101618178A CN 200810115852 A CN200810115852 A CN 200810115852A CN 200810115852 A CN200810115852 A CN 200810115852A CN 101618178 A CN101618178 A CN 101618178A
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- rhizoma curcumae
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Abstract
The invention relates to the application of a curcuma extract in the preparation of medicament for treating Parkinson's disease. The medicament prepared from the curcuma extract for treating Parkinson's disease has advantages of good effect, small dosage and high safety.
Description
Technical field
The present invention relates to Rhizoma Curcumae Longae extract and be used to prepare the application for the treatment of parkinsonian medicine.
Background technology
Parkinson (Parkinson ' s disease, PD) be the chronic progressive external dyskinetic disorder that is common in the old people, clinical manifestation is static tremor, muscle rigidity, bradykinesia and postural reflex obstacle.It is reported that PD is in the crowd more than 60 years old, sickness rate is about 1.5%, and U.S.'s number of patients has 1,000,000 at present, and the number of patients of China surpasses 2,000,000, is only second to the prevalence of diabetes, coronary heart disease, cerebrovascular.Parkinson is the sickness rate height not only, and has more the existing phenomenon that disables in various degree after 2～8 years in morbidity, has a strong impact on patient's quality of life, adds medical expense, has brought mental burden and financial burden for society and family.
Replenishing the interior DA of brain is present the most frequently used and the most effective Therapeutic Method.Early stage at PD, dopamine (DA) single therapy deferrable motor complication and dyskinetic generation are applicable to the patient below 60 years old especially.Exogenous DA can not see through blood brain barrier (BBB), enters in the brain by BBB with its precursor levodopa, is transformed into DA through the DOPA decarboxylase decarboxylation, thereby plays the effect that replenishes DA in the brain.Because DOPA decarboxylase extensively is present in each internal organs of periphery and blood vessel wall, so in drug absorption and transmission course, most of levodopa has been transformed into DA, stimulate periphery DA receptor, cause many-sided untoward reaction, as symptom of digestive tract and cardiovascular symptoms such as blood pressure reduction, arrhythmia such as nauseating, vomiting, anorexia.Be used for the treatment of parkinsonian other medicines and also comprise dopa decarboxylase inhibitor, dopamine-receptor stimulant, monoamine oxidase B inhibitor, catechol-oxygen position-methyltransferase inhibitors etc., but multiple untoward reaction such as these medicines cause nausea in clinical use meeting, vomiting even hepatic injury.Studies show that in recent years, protection DA serotonergic neuron slows down or prevents that the exploitation of nerve protection medicine of the carrying out property degeneration of striatum district DA serotonergic neuron from will become the research focus of Drug therapy PD in future for a long time.
In the prior art, Rhizoma Curcumae Longae as well known to those skilled in the art contains volatile oil 4.5%-6%, and contain in the volatile oil that turmerone (Turmerone) is about 58%, zingerene (Zingerene) is about 25%, phellandrene (Phellandrene) is about 1%, 1,8-cineole (Cineole) is about 1%, sabinene (Sabinene) is about 0.6%, Borneolum Syntheticum (Bomeol) is about 0.5%, dehydroturmerone etc.Contain also that about 0.3%-4.8% of curcumin (Curcumin) and arabinose are about 1.1%, fructose is about 12%, glucose is about 28%, fatty oil, starch, oxalates etc.Rhizome contains curcumin (curcumin) 0.3-1%.And contain demethoxycurcumin (mon-odesmethoxycurcumin, p-hydroxycinnamoyl-feru-loylmethane) and remove dimethoxy curcumin [bis-(p-hydroxycin-namoyl) methane], content is respectively about 4.18% and 3.76%.It is about 4.05% that rhizome still contains volatile oil, and sesquiterpene is about 58%, and zingiberene (zingiberene) is about 25%, and eucalyptol is about 1%, and (d-α-phellandrene) is about 1%, and d-sabinene (d-sabinene) is about 0.6%, Borneolum Syntheticum about 0.5% for d-α-phellandrene.Other contains turmerone (turmerone), ar-turmerone (ar-turmerone) etc.Volatile oil of Rhizoma Curcumae Longae and pigment can be widely different because of the place of production, acquisition time, those skilled in the art it is generally acknowledged December to January next year content the highest.
The Chinese medicine Rhizoma Curcumae Longae is Zingiberaceae curcuma (Curcuma domestica L.) rhizome, curcumin composition (curcumins) in the Rhizoma Curcumae Longae mainly comprises curcumin (curcumin), demethoxycurcumin (demethoxycurcumin) and bisdemethoxycurcumin (bisdemethoxycurcumin), based on curcumin, be the main active of Chinese medicine Rhizoma Curcumae Longae.
Rhizoma Curcumae Longae extract has the merit of removing blood stasis circulation of qi promoting, inducing menstruation to relieve menalgia, is mainly used in diseases such as the twinge of treatment costa sternales, amenorrhea, rheumatism shoulder arm pain, treating swelling and pain by traumatic injury.Studies show that in recent years, Rhizoma Curcumae Longae have antitumor, antioxidation, antiinflammatory, fibrosis, blood fat reducing, mutation, pharmacological action widely such as anticancer, are subjected to the great attention of Chinese scholars.Domestic have more research to the technology of extracting main component from Rhizoma Curcumae Longae at present.Modern age, pharmaceutical research showed, the toxicity of Rhizoma Curcumae Longae extract is very low, LD＞2g/kg of mice, rat oral dose 5g/kg does not observe any toxic and side effects, carry out mtd test with the ICR mice,, do not see animal dead with 600 times of administrations of human oral dosage, and observed every index is all normal, shows that Rhizoma Curcumae Longae extract does not have tangible acute toxicity effect.
Rhizoma Curcumae Longae extract has the function of the multiple disease of quality, and nontoxic, non-evident effect, and application is very extensive, and it mainly acts on is to have the polyphenol structure-activity in the extract.The antiinflammatory that the extract curcumin has, active anticancer fundamentally are the performances of its antioxidant activity.
Parkinsonian pathogenesis is exactly that thereby the dopaminergic neuron degeneration necrosis causes that the DA neurotransmitter levels descends in the substantia nigra of midbrain because the damage of the interior generation of brain oxidative stress causes.Thereby, can eliminate the generation of free radical, the medicine of protection DA serotonergic neuron will have the parkinsonian effect of treatment.
Prior art yet there are no the relevant Rhizoma Curcumae Longae extract that uses and treats parkinsonian purposes.
Summary of the invention
The object of the present invention is to provide Rhizoma Curcumae Longae extract to treat parkinsonian purposes.
Technical scheme of the present invention is that Rhizoma Curcumae Longae extract is used to prepare the purposes that the treatment mammal comprises people's parkinson medicine.Described Rhizoma Curcumae Longae extract extracts from curcuma plant and to obtain.Rhizoma Curcumae Longae extract of the present invention can be prepared into pharmaceutically acceptable dosage form.Described pharmaceutically acceptable dosage form includes, but are not limited to tablet, granule, capsule, oral liquid, injection.
Medicine described in the present invention can also be a kind of pharmaceutical composition, and it comprises Rhizoma Curcumae Longae extract and pharmaceutically acceptable carrier.
Rhizoma Curcumae Longae extract of the present invention is used for the parkinsonian medicine of preparation treatment can be prepared into pharmaceutically any available dosage form.
Utilize Rhizoma Curcumae Longae extract of the present invention to treat parkinsonian effect and can be prepared into the daily health product of taking of people.
The beneficial effect that the present invention has mainly shows as: (1) is compared with the parkinsonian medicine of traditional treatment, has advantage safely and efficiently, and low dose can be brought into play therapeutical effect.(2) crude drug source extensively, be easy to get, cheap.
The present invention also provides a kind of pharmaceutical composition, contains Rhizoma Curcumae Longae extract and pharmaceutically acceptable carrier as active component, for example medicine such as excipient or diluent adjuvant.
Described pharmaceutical composition is after will preparing Rhizoma Curcumae Longae extract and pharmaceutically acceptable medicine adjuvant mixes by ability technical staff known method, according to the conventional preparation method of preparation to prepare required dosage form.Said composition can be liquid preparation forms such as tablet, capsule, granule, or oral liquid or aseptic parenteral solution; Its route of administration, dosage and administration number of times can suitably be adjusted according to patient age, body weight and disease.Common people's consumption is: 200-600mg/ days.
Said composition also can be big or dosage forms such as small-volume injection, freeze-dried powder, aseptic powder packing.
Tablet and capsule that the single agent representation that is used for oral administration can be a Rhizoma Curcumae Longae extract, and can contain conventional excipients, for example syrup, arabic gum, gelatin, sorbitol, tragacanth or polyvinylpyrrolidone such as binding agent; Filler, for example lactose, sugar, corn starch, calcium phosphate, sorbitol or glycine; Tabletting lubricant, for example magnesium stearate; Disintegrating agent, for example starch, polyvinylpyrrolidone, Explotab or microcrystalline Cellulose; Or pharmaceutically acceptable wetting agent, such as sodium lauryl sulphate.
The Rhizoma Curcumae Longae extract solid oral composition can prepare with conventional mixing, filling or pressed disc method.Repeating married operation can be used for activating agent fully is distributed to the compositions of using a large amount of filling doses.Conventional in such operation yes this area.Tablet can make coated tablet or plain sheet according to conventional preparation method.
The Rhizoma Curcumae Longae extract oral liquid can be the form of example emulsion, syrup, perhaps can be used as dry products and exists, and water or other suitable carriers reconstitute again before the use.This liquid preparation can contain conventional additives, such as suspending agent, and for example sorbitol, syrup, methylcellulose, gelatin, hydroxyethyl-cellulose, carboxymethyl cellulose, aluminium stearate gel or hydrogenation edible fat; Emulsifying agent, for example lecithin, anhydro sorbitol-oleate or arabic gum; Anhydrous carrier (can comprise edible oil), for example almond oil, heating up in a steamer Oleum Cocois or oily ester, described oily ester comprises glyceride, propylene glycol or ethanol; Antiseptic, for example methyl parahydroxybenzoate or propyl ester or sorbic acid; If desired, also can add conventional flavoring agent or coloring agent.
For parenteral, particularly injection can be dissolved in the active component Rhizoma Curcumae Longae extract sterile carrier and prepare the unit liquid dosage form.When preparation solution, the active component Rhizoma Curcumae Longae extract can be dissolved in water for injection and filtration sterilization, be filled in bottle or the ampoule afterwards and sealing.Advantageously, adjuvant such as local anesthetic, antiseptic and buffer agent can be dissolved in this carrier.For enhanced stability, recharge in the bottle after can be with said composition freezing, and under vacuum, remove moisture.Or in said composition, comprise surfactant or wetting agent, be beneficial to the uniform distribution of this chemical compound.
The specific embodiment
For the further parkinsonian effect of treatment of research Rhizoma Curcumae Longae extract, the inventor has carried out multiple animal experiment, has obtained gratifying result.
Embodiment 1 Rhizoma Curcumae Longae extract is induced the influence of rotation to apomorphine
Be divided into extract high dose group (70mg/kg) after the bull healthy SD rat injection 6-OHDA 15 μ g modelings success, middle dosage group (35mg/kg), low dose group (17.5mg/kg), positive drug (L-levodopa) group (140mg/kg), every day, the difference gastric infusion was 1 time.Other establishes normal control group, model group and sham operated rats, gives equivalent 0.5%CMC water.Continuous 1 week.
Adopt the filling stomach to give rat commercially available (Hebei Food Addiitive Co., Ltd., No. 55, street, the Kunlun, Shijiazhuang City, Hebei Province city) Rhizoma Curcumae Longae extract, can obviously reduce number of revolutions after 7 days, wherein high dose 70mg/kg group and middle dosage 35mg/kg group have obvious significant difference (P＜0.05), identical with the effect of positive drug levodopa (P＜0.05), and the dosage of extract only is the 1/4-1/2 of levodopa.Concrete outcome is as shown in table 1 below:
Table 1 Rhizoma Curcumae Longae extract is induced the influence of rat rotation to apomorphine
###Compare with sham operated rats P＜0.001;
*Compare with model group P＜0.05.
Rhizoma Curcumae Longae extract is to the influence of rat balanced capacity
Rat is placed on the sintering in the face of the mouse cage direction, picks up counting simultaneously, pass by time (incubation period) of sintering and rat of record rat passed by time of the whole gimbal lever, and the maximum permission time of incubation period is 1min, and the cross bar maximum permission time of passing by is 2min.Rat training earlier 3 times begins formal experiment then.
The motion initiating of model mouse and moving equilibrium ability are all obviously than sham operated rats difference (P＜0.05, P＜0.01).Irritate the stomach treatment after 7 days through extract, the rat motor coordination ability all has clear improvement (P＜0.01), and wherein high dose group is to action effect the best (P＜0.001) of moving equilibrium ability.The positive drug effect (P＜0.01) that also has clear improvement.Concrete outcome is seen Fig. 2, Fig. 3.
Table 2 is respectively organized rat gimbal lever experimental result incubation period
#Compare with sham operated rats P＜0.05;
*Compare with model group P＜0.01.
Table 3 is respectively organized the rat gimbal lever and is crossed the bar interpretation
##Compare with sham operated rats P＜0.01;
*P＜0.01,
* *Compare with model group P＜0.001.
Embodiment 2 Rhizoma Curcumae Longae extracts are to the influence of spontaneous activity in mice
The C57BL/6 mice be divided into matched group, model group, low dose therapy group (25mg/kg), middle dosage treatment group (50mg/kg), high-dose therapy group (100mg/kg), positive drug group (levodopa, 200mg/kg).Model group, each group of treatment and positive drug group mice are with the dosage lumbar injection of MPTP 15mg/kg 4 times.After modeling the 1st day, medication therapy groups, positive drug group mice were irritated stomach respectively 1 time with 0.1ml/10g every day, and matched group and model group are given equivalent 0.5%CMC water, a continuous week.Modeling and after 1 week of administration, each group are carried out autonomic movement and bull stick respectively and are observed.
Rhizoma Curcumae Longae extract successive administration 7 days under 100mg/kg dosage, model mice spontaneous activity number of times obviously increases (P＜0.05), Rhizoma Curcumae Longae extract is at 25mg/kg, and successive administration is 7 days under 50mg/kg and the 100mg/kg dosage, makes model mice bull stick movement time obviously prolong (P＜0.05).The effect of Rhizoma Curcumae Longae extract and positive drug levodopa are approaching, but dosage reduces.The results are shown in Table 4.
Table 4 Rhizoma Curcumae Longae extract is to the ethological influence of parkinson mouse model
#P＜0.05,
##Compare with matched group P＜0.01;
*P＜0.05,
*Compare with model group P＜0.01.
Rhizoma Curcumae Longae extract is used to prepare pharmaceutically, and the embodiment of any available dosage form includes, but are not limited to following examples.
Embodiment 3
According to method well known to those skilled in the art, with commercially available Rhizoma Curcumae Longae extract, after adjuvant mixes, be filled directly into capsule, every capsules contains Rhizoma Curcumae Longae extract 0.5g.
Embodiment 4
According to method well known to those skilled in the art, commercially available Rhizoma Curcumae Longae extract is added appropriate amount of starch, be pressed into tablet, wherein Rhizoma Curcumae Longae extract 0.3g.
Embodiment 5
According to method well known to those skilled in the art, commercially available Rhizoma Curcumae Longae extract is pulverized, add an amount of sucrose Icing Sugar, granulate with the moistening back of 75% ethanol water, oven dry, the preparation granule, the content of Rhizoma Curcumae Longae extract is 1g.
Embodiment 6
According to method well known to those skilled in the art,, make injection with commercially available Rhizoma Curcumae Longae extract and glucose or normal saline wiring solution-forming.The content of Rhizoma Curcumae Longae extract is 0.1g.
Embodiment 7
According to method well known to those skilled in the art, Rhizoma Curcumae Longae extract with after adjuvant mixes, is filled directly into capsule, make it every capsules and be equivalent to 1.0g Rhizoma Curcumae Longae raw medicinal herbs, perhaps make spansule.
Embodiment 8
According to method well known to those skilled in the art, according to method well known to those skilled in the art, commercially available Rhizoma Curcumae Longae extract is added in the sucrose solution, contain the 0.5g extract in every ml soln, make oral liquid.
Claims (6)
1, Rhizoma Curcumae Longae extract is used to prepare the purposes that the treatment mammal comprises people's parkinson medicine.
2, purposes according to claim 1 is characterized in that Rhizoma Curcumae Longae extract extracts to obtain from curcuma plant.
3, purposes according to claim 1 is characterized in that Rhizoma Curcumae Longae extract contains curcumin, demethoxycurcumin and bisdemethoxycurcumin.
4,, it is characterized in that described medicine comprises Rhizoma Curcumae Longae extract and pharmaceutically acceptable carrier according to each described purposes of claim 1-3.
5,, it is characterized in that described Rhizoma Curcumae Longae extract is prepared into pharmaceutically acceptable dosage form according to each described purposes of claim 1-3.
6,, it is characterized in that described pharmaceutically acceptable dosage form comprises tablet, granule, capsule, oral liquid, injection according to each described purposes of claim 1-3.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN200810115852A CN101618178A (en) | 2008-06-30 | 2008-06-30 | Application of curcuma extract in preparation of medicament for treating Parkinson's disease |
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| CN200810115852A CN101618178A (en) | 2008-06-30 | 2008-06-30 | Application of curcuma extract in preparation of medicament for treating Parkinson's disease |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111838662A (en) * | 2020-07-31 | 2020-10-30 | 广西天缘绿生物科技有限公司 | High negative potential plantain fruit extract |
| WO2022052016A1 (en) * | 2020-09-11 | 2022-03-17 | Liu Hsuan Miao | Pharmaceutical compositions and uses thereof in treating parkinson's disease |
-
2008
- 2008-06-30 CN CN200810115852A patent/CN101618178A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111838662A (en) * | 2020-07-31 | 2020-10-30 | 广西天缘绿生物科技有限公司 | High negative potential plantain fruit extract |
| WO2022052016A1 (en) * | 2020-09-11 | 2022-03-17 | Liu Hsuan Miao | Pharmaceutical compositions and uses thereof in treating parkinson's disease |
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Open date: 20100106 |